Ambrisentanisapropanoicacidbased,orally-available,endothelinreceptortypeA-receptorantagoNISTfortheonce-dailytreatmentofpulmonaryarterialhypertension(PAH).Ithas>4000-foldselectivityforthetypeAreceptorovertypeBreceptor.StudiesindicatethatAmbrisentanhasalowpotentialfordruginteractionsandattherapeuticconcentrationsdoesnotinhibitUDP-glucuronosyltransferasesorCYPs,orinduceMDRprotein2orP-gp.(1)
Incontrastwithothersimilartherapies,Ambrisentanhasbeenshowntohavealowerpotentialforincreaseofserum-levelconcentrationsofaminotransferases.(2)
Technicalinformation:
| ChemicalFormula: | C22H22N2O4 | |
| CAS#: | 177036-94-1 | |
| MolecularWeight: | 378.42 | |
| Purity: | >98% | |
| Appearance: | white | |
| ChemicalName: | (S)-2-((4,6-dimethylpyrimidin-2-yl)oxy)-3-methoxy-3,3-diphenylpropanoicacid | |
| Solubility: | Upto100mMinDMSO | |
| Synonyms: | LU-208075,BSF-208075 |
ShippingCondition:Theproductisshippedinaglassvialatambienttemperature.
Storagecondition:Forlongershelflife,storesolidpowderat4oCdesiccated,orstoreDMSOsolutionat-20oC.
Reference:
| 1. | Frampton,JE.,Ambrisentan.Am.J.Cardiovasc.Drugs2011,11(4),215-226.PubmedID:21623643 |
| 2. | Galieetal.,ResultsoftheAmbrisentaninPulmonaryArterialHypertension,Randomized,Double-Blind,Placebo-Controlled,Multicenter,Efficacy(ARIES)Study1and2.Circulation,2008,117,3010-3019.PubmedID:18506008 |